Benicar - General Information
Benicar belongs to the class of medicines called angiotensin II receptor antagonists to treat high blood pressure. It is marketed worldwide by Daiichi Sankyo, Ltd. and in the United States by Daiichi Sankyo, Inc. and Forest Laboratories.
Pharmacology of Benicar
Benicar, a specific angiotensin II type 1 antagonist, is used alone or with other antihypertensive agents to treat hypertension. Unlike the angiotensin receptor antagonist losartan, olmesartan does not have an active metabolite or possess uricosuric effects. Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and circulating angiotensin II levels do not overcome the effect of olmesartan on blood pressure.
Benicar for patients
Pregnancy: Female patients of childbearing age should be told about the consequences of second and third trimester exposure to drugs that act on the renin-angiotensin system and they should be told also that these consequences do not appear to have resulted from intrauterine drug exposure that has been limited to the first trimester. These patients should be asked to report pregnancies to their physicians as soon as possible.
No significant drug interactions were reported in studies in which olmesartan medoxomil was co-administered with digoxin or warfarin in healthy volunteers. The bioavailability of olmesartan was not significantly altered by the co-administration of antacids [Al(OH)3/Mg(OH)2]. Olmesartan medoxomil is not metabolized by the cytochrome P450 system and has no effects on P450 enzymes; thus, interactions with drugs that inhibit, induce or are metabolized by those enzymes are not expected.
Benicar is contraindicated in patients who are hypersensitive to any component of this product.
Additional information about Benicar
Benicar Indication: For the treatment of hypertension
Mechanism Of Action: Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation and renal reabsorption of sodium. Benicar blocks the vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in vascular smooth muscle. Its action is, therefore, independent of the pathways for angiotensin II synthesis. Benicar has more than a 12,500-fold greater affinity for the AT1 receptor than for the AT2 receptor.
Drug Interactions: Drospirenone Increased risk of hyperkaliemia
Food Interactions: Food does not affect the bioavailability of olmesartan.
Generic Name: Olmesartan
Synonyms: Olmesartan medoximil; Olmesartan medoxomil
Drug Category: Angiotensin II Type 1 Receptor Blockers; Antihypertensive Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Olmesartan: Benicar; Olmetec; Votum;
Absorption: Bioavailability is about 26%. Food does not affect the bioavailability of olmesartan.
Toxicity (Overdose): Symptoms of overdose include dehydration (dry mouth, excessive thirst, muscle pain or cramps, nausea and vomiting, weakness), dizziness, low blood pressure, and slow or irregular heartbeat.
Protein Binding: Highly bound to plasma proteins (99%) and does not penetrate red blood cells.
Biotransformation: Olmesartan is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract. There is virtually no further metabolism of olmesartan.
Half Life: Approximately 13 hours
Dosage Forms of Benicar: Tablet Oral
Chemical IUPAC Name: (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate
Chemical Formula: C29H30N6O6
Olmesartan on Wikipedia: http://en.wikipedia.org/wiki/Olmesartan
Organisms Affected: Humans and other mammals